Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators.
A series of amides, structurally related to DM232 (unifiram) and DM235 (sunifiram), characterized by a 1,2,3,4-tetrahydropyrazino[2,1-a]isoindol-6(2H)-one, 1,4-diamino-cyclohexane or 1,4-diaminobenzene ring, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, while some cyclohexane derivatives are endowed with amnesia inducing properties.
Martini
Elisabetta
E
Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy.
Norcini
Monica
M
Ghelardini
Carla
C
Manetti
Dina
D
Dei
Silvia
S
Guandalini
Luca
L
Melchiorre
Michele
M
Pagella
Simona
S
Scapecchi
Serena
S
Teodori
Elisabetta
E
Romanelli
Maria Novella
MN
D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects / Q000502:physiology; D003627:Data Interpretation, Statistical; D015195:Drug Design; D051379:Mice; D018697:Nootropic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology; D021641:Recognition, Psychology / Q000187:drug effects
D018697:Nootropic Agents; D010879:Piperazines; D011758:Pyrroles; C416655:DM 235; C409868:DM 232